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Last Updated: December 28, 2024

Claims for Patent: 7,759,308

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Summary for Patent: 7,759,308

Title:	Microparticles comprising somatostatin analogues
Abstract:	Disclosed are microparticles comprising a somatostatin analogue embedded in a biocompatible pharmacologically acceptable polymer matrix for a long acting release and pharmaceutical compositions comprising such microparticles.
Inventor(s):	Ahlheim; Markus (Staufen, DE), Ausborn; Michael (Lorrach, DE), Lambert; Olivier (Spechbach-le-Haut, FR), Riemenschnitter; Marc (Freiburg, DE)
Assignee:	Novartis AG (Basel, CH)
Application Number:	10/579,186
Patent Claims:	1. Microparticles comprising cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] in free form, salt form or protected form embedded in a polymer matrix wherein the polymer matrix comprises a linear and a star polylactide-co-glycolide. 2. Microparticles according to claim 1 wherein the cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] is in pamoate salt form. 3. Microparticles according to claim 1 wherein the polymer matrix comprises a linear polylactide-co-glycolide polymer and a star polylactide-co-glycolide polymer having a weight average molecular weight of about 50,000 Da. 4. Microparticles according to claim 1 wherein the ratio of linear to star polylactide-co-glycolide is 50:50. 5. Microparticles according to claim 1 wherein the cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] is an amourphous powder having a particle size less than about 5 microns. 6. Microparticles according to claim 1 further comprising a surfactant, a porosity influencing agent and/or a basic salt. 7. A pharmaceutical composition comprising microparticles according to claim 1 and a water-based vehicle comprising a wetting agent. 8. A composition according to claim 7 wherein the wetting agent comprises a poloxamer and/or a polyoxyethylene-sorbitan-fatty acid ester. 9. A composition according to any one of claim 7 wherein the vehicle comprises a tonicity agent. 10. A composition according to any one of claim 7 wherein the vehicle comprises a viscosity increasing agent. 11. A kit comprising microparticles according to claim 1 and a water-based vehicle.

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